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. 2012 Nov 29;4(2):255–260. doi: 10.1021/cn300180a

Table 1. Memantine and Amantadine IC50, (Amantadine IC50)/(Memantine IC50) Ratio, Ω, and ΔΔG° for Wild Type and Mutant NMDA Receptorsa.

  memantine IC50 (μM) N amantadine IC50 (μM) N IC50 ratio Ω ΔΔG°
WT 0.54 ± 0.03 18 41 ± 5.6 6 75    
GluN1 mutants
N616Q 5.9 ± 0.5 6 490 ± 73 10 83 1.1 –0.06
N616D 14 ± 1.3 7 590 ± 21 5 41 0.55 0.35
V644N 12 ± 3.2 7 150 ± 27 8 12 0.16 1.1
V644T 0.26 ± 0.06 13 44 ± 15 13 170 2.2 –0.48
V644L 0.26 ± 0.09 15 26 ± 6.5 11 100 1.3 –0.17
A645N 240 ± 16 11 1000 ± 68 11 4.4 0.06 1.7
A645L 4.8 ± 0.4 9 53 ± 4.4 9 11 0.15 1.1
A645V 0.60 ± 0.06 9 21 ± 0.8 14 34 0.46 0.47
V656N 2.4 ± 0.2 8 94 ± 14 7 40 0.53 0.38
GluN2B mutants
N615D 1.3 ± 0.3 7 300 ± 17 9 230 3.1 –0.67
N616D 1.0 ± 0.1 6 56 ± 5.3 10 55 0.74 0.18
A639N 3.6 ± 0.4 10 140 ± 26 11 39 0.51 0.39
V640N 0.29 ± 0.03 11 12 ± 2.6 8 42 0.55 0.35
L643N 34 ± 2.7 10 750 ± 130 13 22 0.29 0.73
A644N 90 ± 2.0 9 340 ± 29 10 3.7 0.05 1.8
A644L 0.29 ± 0.07 12 3.6 ± 0.4 12 12 0.17 1.0
A644V 0.41 ± 0.05 14 10. ± 0.7 11 25 0.33 0.66
a

N= number of cells. IC50 ratio = IC50(amantadine)/IC50(memantine). Ω = [(wild type memantine IC50)(mutant amantadine IC50)]/[wild type amantadine IC50)/(mutant memantine IC50)]. ΔΔG0 = RT ln(Ω), where R = 1.987 kcal·mol–1·K–1 and T = 298 K.